1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid | 329014-26-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
• 英文别名: 1-(6-Amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-4-oxoquinoline-3-carboxylic acid
• CAS: 329014-26-8
• 化学式: C₁₉H₁₅F₃N₄O₄
• 分子量: 420.348
• InChiKey: QAURAGVLTXYSIZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  120
• 氢给体数：
  3
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  1-(6-amino-3,5-difluoropyridin-2-yl)-6,7-difluoro-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 、 3-羟基氮杂环丁烷盐酸盐 在 lithium hydroxide 、 氯化镁 、 柠檬酸 作用下， 以 吡啶 、 乙醇 、 水 、 二甲基亚砜 为溶剂， 生成 1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
  参考文献：
  名称：

  Quinolinecarboxylic acid derivative or its salt

  摘要：

  本发明涉及一种1-(6-氨基-3,5-二氟吡啶-2-基)-6-氟-7-(3-羟基氮杂环戊烷-1-基)-8-甲基-1,4-二氢-4-氧喹诺酮-3-羧酸或其盐；以及含有该化合物作为活性成分的药物。由于该化合物或其盐对光高度稳定，同时保持喹诺酮类抗菌剂固有的优良特性，因此，包含该发明化合物或其盐作为活性成分的抗菌剂可以长时间存储，而不会出现药效降低，因此可以作为稳定的制剂，如注射剂、眼药水和外科药品供应。

  公开号：

  US06586420B1

文献信息

• QUINOLINECARBOXYLIC ACID DERIVATIVE OR ITS SALT
  申请人：WAKUNAGA PHARMACEUTICAL CO., LTD.

  公开号：EP1219618A1

  公开（公告）日：2002-07-03

  The present invention relates to a 1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or salt thereof; and drugs containing the same as the active ingredient. Since this compound or salt thereof is highly stable to light while sustaining the excellent properties inherent to quinolone antibacterial agents, an antibacterial agent comprising, as an active ingredient, the invention compound or salt thereof can be stored over a long period of time without suffering from any decrease in the drug effect and can therefore be supplied as stable preparations such as injections, eye drops and surgical medicines.

  本发明涉及一种 1-(6-氨基-3,5-二氟吡啶-2-基)-6-氟-7-(3-羟基氮杂环丁烷-1-基)-8-甲基-1,4-二氢-4-氧代喹啉-3-羧酸或其盐，以及以其为活性成分的药物。由于这种化合物或其盐对光高度稳定，同时又保持了喹诺酮类抗菌剂固有的优良特性，因此含有本发明化合物或其盐作为有效成分的抗菌剂可以长期储存而不会降低药效，因此可以作为注射剂、滴眼剂和手术药物等稳定制剂供应。
• EP1219618A4
  申请人：——

  公开号：EP1219618A4

  公开（公告）日：2002-09-18
• PHARMACEUTICAL COMPOSITION
  申请人：NAKAGAMI Hiroaki

  公开号：US20110159049A1

  公开（公告）日：2011-06-30

  The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube.
• US6586420B1
  申请人：——

  公开号：US6586420B1

  公开（公告）日：2003-07-01
• [EN] QUINOLINECARBOXYLIC ACID DERIVATIVE OR ITS SALT<br/>[FR] DERIVE D'ACIDE QUINOLINECARBOXYLIQUE OU SON SEL
  申请人：WAKUNAGA PHARMA CO LTD

  公开号：WO2001017991A1

  公开（公告）日：2001-03-15

  1-(6-Amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or its salt, and drugs containing the same as the active ingredient. Since this compound and its salt are highly stable to light while sustaining the excellent properties inherent to quinolone antibiotics, antibacterial agents containing the same can be stored over a long period of time without suffering from any decrease in the drug effect. Thus, these drugs can be supplied as stable preparations such as injections, eye drops and surgical medicines.